- Towards the synthesis of osteoclast inhibitor SB-242784
-
Osteoclast inhibitor SB-242784 (1) was prepared from pivotal indol intermediate 4. A 'Stille' cross coupling of organotin 2c with bromo acrylate 11 afforded diene 12 which was also obtained via a reduction-isomerization process of enyne 16. Bromoamide 3 was prepared from the corresponding acid 7 which was readily obtained from bromopyruvic acid.
- Conde, Jose J.,McGuire, Michael,Wallace, Michael
-
p. 3081 - 3084
(2007/10/03)
-
- Aminotetralin derivatives
-
This invention related to new aminotetralin derivatives of formula I STR1 wherein STR2 B is methylene or, when A is --CH2 --CH2 --, --CH=CH--, --NH--CO-- or --CH2 --CO--, B can also be carbonyl or thiocarbonyl; E is a C2 -C4 straight-chain alkylene, optionally substituted by a C1 -C3 alkyl, or is 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene; R1 is hydrogen, fluorine, chlorine, bromine, trifluoromethyl, nitro, amino, C1 -C3 alkylamino, C1 -C3 dialkylamino, C1 -C3 alkyl, C1 -C3 alkylthio, hydroxy, C1 -C3 alkoxy or phenyl C1 -C3 alkoxy; R2 is hydrogen, chlorine, bromine, hydroxy, C1 -C3 alkoxy phenyl C1 -C3 alkoxy, or C1 -C3 alkyl or, together with R1, can be a C1 -C2 alkylenedioxy; R3 and R4 are each independently selected from hydrogen, fluorine, chlorine, bromine, C1 -C3 alkyl, hydroxy, C1 -C3 alkoxy, nitro, amino, C1 -C3 alkylamino, or C1 -C3 dialkylamino, or together can be methylenedioxy; and R5 is hydrogen, C3 -C5 alkenyl, C1 -C3 alkyl, or phenyl C1 -C3 alkyl, and nontoxic, pharmaceutically acceptable addition salts thereof which have valuable pharmacological properties, particularly a long-lasting heart rate lowering effect and the effect of reducing the O2 requirement of the heart.
- -
-
-